HRP20230279T1 - Benzenesulfonyl-asymmetric ureas and medical uses thereof - Google Patents

Benzenesulfonyl-asymmetric ureas and medical uses thereof Download PDF

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HRP20230279T1
HRP20230279T1 HRP20230279TT HRP20230279T HRP20230279T1 HR P20230279 T1 HRP20230279 T1 HR P20230279T1 HR P20230279T T HRP20230279T T HR P20230279TT HR P20230279 T HRP20230279 T HR P20230279T HR P20230279 T1 HRP20230279 T1 HR P20230279T1
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pharmaceutically acceptable
acceptable salt
compound according
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HRP20230279TT
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Croatian (hr)
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Claudio Giuliano
Antoine Daina
Claudio Pietra
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Helsinn Healthcare S.A.
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    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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Claims (22)

1. Spoj formule IV: [image] ili njegova farmaceutski prihvatljiva sol, gdje: isprekidana linija označava izbornu vezu; X je veza, CO ili CR7R8; k je 0-2; Z je halo, metoksi ili C1-3 alkil izborno supstituiran sa halo; R1 i R2 su svaki neovisno, H, C1-3 alkil, metoksi, halo ili OH; ili R1 i R2 uzeti zajedno sa atomima za koje su vezani formiraju 5-6 -člani prsten; ili R1 i X uzeti zajedno sa atomima za koje su vezani formiraju 5-6 -člani prsten; R3 je H, C1-3 alkil, metoksi, halo, OH, COOR12, CR13R14OH, COHNR15, cikloalkil ili heteroaril; R4 je veza ili CR9R10; U je C, N, S ili O; R’ je halo, heteroaril, C1-6 alkoksi, C1-6 alkil, heterocikloalkil, CN cikloalkil, CO2(C1-6 alkil) ili CO(C1-6 alkil); ili dva R’ uzeti zajedno sa atomima za koje su vezani formiraju 5-6 -člani prsten; R7 i R8 su svaki, neovisno, H ili C1-3 alkil, ili CONH2, pri čemu navedeni C1-3 alkil je izborno supstituiran sa halo; R9 i R10 su svaki, neovisno, H ili C1-3 alkil, pri čemu navedeni C1-3 alkil je izborno supstituiran sa halo; R12, R13, R14 i R15 su svaki neovisno H ili C1-3 alkil. R16 je H ili C1-3 alkil; R17 je H, halo, ili C1-3 alkil; l je 0-3; m je 0-3; n je 0-3, i p je 1-3.1. Compound of formula IV: [image] or a pharmaceutically acceptable salt thereof, where: dashed line indicates optional connection; X is a bond, CO or CR7R8; k is 0-2; Z is halo, methoxy or C1-3 alkyl optionally substituted with halo; R 1 and R 2 are each independently, H, C 1-3 alkyl, methoxy, halo or OH; or R1 and R2 taken together with the atoms to which they are attached form a 5-6 membered ring; or R1 and X taken together with the atoms to which they are attached form a 5-6 membered ring; R 3 is H, C 1-3 alkyl, methoxy, halo, OH, COOR 12 , CR 13 R 14 OH, COHNR 15 , cycloalkyl or heteroaryl; R4 is a link or CR9R10; U is C, N, S or O; R' is halo, heteroaryl, C1-6 alkoxy, C1-6 alkyl, heterocycloalkyl, CN cycloalkyl, CO2(C1-6 alkyl) or CO(C1-6 alkyl); or two R' taken together with the atoms to which they are attached form a 5-6-membered ring; R 7 and R 8 are each, independently, H or C 1-3 alkyl, or CONH 2 , wherein said C 1-3 alkyl is optionally substituted with halo; R 9 and R 10 are each, independently, H or C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted with halo; R 12 , R 13 , R 14 and R 15 are each independently H or C 1-3 alkyl. R 16 is H or C 1-3 alkyl; R 17 is H, halo, or C 1-3 alkyl; l is 0-3; m is 0-3; n is 0-3, and p is 1-3. 2. Spoj prema patentnom zahtjevu 1, naznačen time što p je 1 ili 2.2. A compound according to claim 1, characterized in that p is 1 or 2. 3. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, izabrani iz grupe koja se sastoji od sljedećih: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] 3. The compound according to claim 1 or its pharmaceutically acceptable salt, selected from the group consisting of the following: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] 4. Spoj prema patentnom zahtjevu 1, izabran iz grupe koja se sastoji od: [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] [image] , [image] , [image] , [image] , [image] , ili njegova farmaceutski prihvatljiva sol.4. Compound according to claim 1, selected from the group consisting of: [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] [image] , [image] , [image] , [image] , [image] , or a pharmaceutically acceptable salt thereof. 5. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.5. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 6. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.6. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 7. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.7. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 8. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.8. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 9. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.9. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 10. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.10. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 11. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.11. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 12. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.12. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 13. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.13. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 14. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.14. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 15. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.15. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 16. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.16. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 17. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.17. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 18. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.18. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 19. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.19. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 20. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.20. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 21. Spoj prema patentnom zahtjevu 1, koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.21. Compound according to patent claim 1, which has the structure: [image] or a pharmaceutically acceptable salt thereof. 22. Spoj formule IV prema bilo kojem od patentnih zahtjeva 1-21, za uporabu u prevenciji i/ili liječenju bolesti koja je patofiziološki povezana sa receptorom grelina kod subjekta.22. A compound of formula IV according to any one of claims 1-21, for use in the prevention and/or treatment of a disease that is pathophysiologically related to the ghrelin receptor in a subject.
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